Assay Detail
Functional
CHEMBL864503
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Antagonist activity at human cloned CLR/RAMP1 receptor expressed in E10 cells measured as inhibition of CGRP-mediated cAMP production
11
Total Activities
9
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | E10 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 (CHEMBL2107838) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.69 | 10.00 |
| Kb | 1 | - | - |
| Kd | 1 | 7.10 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL207197 | OLCEGEPANT | 2.0 | 1 | 10.00 |
| CHEMBL424864 | — | — | 3 | 7.42 |
| CHEMBL381710 | — | — | 1 | 7.37 |
| CHEMBL381585 | — | — | 1 | 7.12 |
| CHEMBL211052 | — | — | 1 | 6.00 |
| CHEMBL381798 | — | — | 1 | 5.80 |
| CHEMBL380514 | — | — | 1 | 5.74 |
| CHEMBL207186 | — | — | 1 | 5.44 |
| CHEMBL379686 | — | — | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL207197 | OLCEGEPANT | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL424864 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL381710 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL381585 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL424864 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL211052 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL381798 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL380514 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL207186 | — | IC50 | = | 3640.0 | nM | 5.44 |
| CHEMBL379686 | — | IC50 | = | 4450.0 | nM | 5.35 |
| CHEMBL424864 | — | Kb | = | 77.0 | nM | - |